December 2018 Poison Center Hotline: 1-800-222-1222

The Maryland Poison Center’s Monthly Update: News, Advances, Information Tianeptine Tianeptine is an atypical tricyclic antidepressant used in Europe, Asia and Latin America. It has antidepressant and anxiolytic properties. While its structure is similar to that of tricyclic antidepressants, its pharmacologic profile is different. Tianeptine enhances serotonin reuptake and modulates neuroplasticity in the hippocampus, amygdala and prefrontal cortex. As tianeptine is also a mu opioid receptor agonist, there is concern about its potential for abuse. Tianeptine is not approved by the Food and Drug Administration (FDA) for use in the U.S. but is available online as a research chemical or as a dietary supplement or cognitive enhancer. Since the FDA has not approved it for any use, dietary supplements containing tianeptine are considered adulterated with an unsafe food additive. Unproven claims that it can treat opioid use disorder, pain, stress, Did you know? and other ailments are illegal. In November 2018 the FDA posted warning letters to two companies for illegal marketing of tianeptine-containing dietary supple- Anyone can submit a report ments (https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ regarding product safety ucm626349.htm). concerns. Case reports of tianeptine misuse and abuse describe similar effects as opioids The FDA and National Institutes of and use of naloxone with positive response. Acute toxic effects include agitation, Health (NIH) have an on-line Safety sedation, respiratory depression, miosis and arrhythmias. A literature review Reporting Portal for issues conducted in 2018 found 25 articles involving 65 patients with tianeptine abuse regarding food, medicines, dietary or dependence (Psychosomatics. July 19,2018; E-pub ahead of print). The majority supplements, and other products. of cases (53) were outside the U.S. Three quarters of patients were male and Some organizations and under the age of 35 years. The average daily dose was close to 2 grams, far professionals are required by law above the usual therapeutic dose of 25-50 mg daily. Routes of administration to submit reports. Health care included oral, intravenous and insufflation. There were 9 deaths, three of which providers, other professionals and involved at least one other substance. Another 2018 literature review of 18 pa- consumers/concerned citizens may tients observed a prior history of substance abuse in 72%. Doses were well voluntarily submit reports above therapeutic with a mean of 1469 mg/day and as high as 4125 mg/day (J regarding safety and/or Psychoactive Drugs 2018;50:275-80). The Centers for Disease Control and Preven- unanticipated harmful effects of tion (CDC) analyzed 218 tianeptine exposure calls reported to poison control products. Use this link for centers in the U.S. from 2000 to 2017 (MMWR 2018;67:815-8). From 2000 to 2013 there were only 11 calls; the increase in calls and in intentional abuse or reporting: https:// misuse from 2014-2017 was statistically significant. The mean age was 35 years www.safetyreporting.hhs.gov . with the majority of cases involving persons 21-40 years. Most common clinical effects in the 114 tianeptine-only exposures (excluding withdrawal related calls) were neurologic (48%), cardiovascular (32.5%) and gastrointestinal (10.5%). The most common co-exposures in 83 patients with other substances were Wendy Klein-Schwartz, PharmD, MPH, FAACT phenibut, ethanol, benzodiazepines and opioids. Professor Emeritus University of Maryland School of Pharmacy Chronic tianeptine users develop dependence and withdrawal symptoms that are similar to those of opioid withdrawal. In the CDC study referenced above, there were 21 tianeptine-only withdrawal calls to poison centers. The most fre- quently reported effects in these patients were agitation, nausea, vomiting, tachycardia, hypertension, diarrhea, tremor and diaphoresis. @MPCToxTidbits

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